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Completed

NCT Number: NCT04902105

Drug-Drug Interaction Study to Evaluate the Effect of Inhibition of UGTs on the PK of Ecopipam and Its Active Metabolite

This is a single center, open-label, fixed sequence, drug-drug interaction (DDI) study in healthy subjects.

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Key information

Conditions

Drug Interaction

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Syneos Health Clinical Research Services, LLC.

Miami, Florida, 33136, United States

About this study

Following a 28-day Screening period, eligible subjects will enter the clinical research unit (CRU) and will be enrolled into either Cohort A or B. Subjects in both cohorts will receive a single dose of ecopipam on Day 1. On Day 7, subjects will begin taking a UGT inhibitor according to their assigned cohort. Subjects in Cohort A will receive mefenamic acid 250 mg every 6 hours for 7 days, while subjects in Cohort B will receive divalproex sodium ER 1250 mg once a day for 10 days. A single oral dose of ecopipam will also be administered to Cohort A on Day 7, 1 hour after the first dose of mefenamic acid, and to Cohort B on Day 10, 1 hour after administration of divalproex sodium ER. Subjects in Cohort A will continue taking mefenamic acid through the evening of Day 13 and will remain in the CRU until discharged on Day 14/ET. Subjects in Cohort B will continue taking divalproex sodium ER through Day 16 and will remain in the CRU until discharge on Day 17/ET.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Male subjects or female subjects of non-childbearing potential
  • ≥18 and ≤55 years of age at the time of consent
  • BMI >18.5 and <30 kg/m2 and a weight of ≥50 kg
  • Sexually active males must use a double barrier method of contraception during the study and for at least 90 days after the last dose of study drug
  • Male subjects must be willing not to donate sperm until 90 days following the last study drug administration

Exclusion criteria

  • Personal or family History of significant medical illness
  • Clinically significant abnormalities on screening tests/exams
  • History of or significant risk of committing suicide
  • Donation of plasma within 7 days prior to dosing
  • Donation or significant loss of blood within 30 days prior to the first dosing
  • Major surgery within 3 months or minor surgery within 1 month prior to admission
  • Use of prohibited prescription, over-the-counter medications or natural health products
  • Alcohol-based products 24 hours prior to admission
  • Female subjects who are currently pregnant or lactating
  • Use of tobacco or nicotine products within 3 months prior to Screening
  • Significant alcohol consumption
  • History of drug abuse within the previous 2 years, or a positive drug screen
  • History of allergy to study medications
  • Not suitable for study in the opinion of the Principal Investigator

Treatment and study plan

ecopipam HCL

Drug

oral tablets

mefenamic acid

Drug

oral capsules

divalproex sodium ER

Drug

oral tablets

Primary outcomes

  1. Cmax of ecopipam in the presence of mefenamic acid

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  2. Cmax of ecopipam in the absence of mefenamic acid

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  3. Cmax of ecopipam in the presence of divalproex sodium ER

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  4. Cmax of ecopipam in the absence of divalproex sodium ER

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  5. AUCinf of ecopipam in the presence of mefenamic acid

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  6. AUCinf of ecopipam in the absence of mefenamic acid

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  7. AUCinf of ecopipam in the presence of divalproex sodium ER

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  8. AUCinf of ecopipam in the absence of divalproex sodium ER

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  9. AUC0-143 of ecopipam in the presence of mefenamic acid

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  10. AUC0-143 of ecopipam in the absence of mefenamic acid

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  11. AUC0-143 of ecopipam in the presence of divalproex sodium ER

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  12. AUC0-143 of ecopipam in the absence of divalproex sodium ER

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

Secondary outcomes

  1. Cmax of EBS-101-40853

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  2. AUCinf of EBS-101-40853

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  3. AUC0-143 of EBS-101-40853

    Time frame: Up to Day 16

    Up to 35 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  4. Cmax of mefenamic acid

    Time frame: Up to Day 16

    Up to 15 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  5. Tmax of mefenamic acid

    Time frame: Up to Day 16

    Up to 15 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  6. AUCtau of mefenamic acid

    Time frame: Up to Day 16

    Up to 15 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  7. t½ of mefenamic acid

    Time frame: Up to Day 16

    Up to 15 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  8. Cmax of VPA

    Time frame: Up to Day 16

    Up to 19 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  9. Tmax of VPA

    Time frame: Up to Day 16

    Up to 19 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  10. AUCtau of VPA

    Time frame: Up to Day 16

    Up to 19 blood samples will be collected at the indicated time points for pharmacokinetic analysis

  11. Safety and tolerability as demonstrated by MOAA/S

    Time frame: Up to Day 17

    Safety and tolerability measures will be recorded at the indicated timepoints.

  12. Safety and tolerability as demonstrated by C-SSRS

    Time frame: Up to Day 17

    Safety and tolerability measures will be recorded at the indicated timepoints.

  13. Safety and tolerability as demonstrated by concomitant medications

    Time frame: Up to Day 42

    Safety and tolerability measures will be recorded at the indicated timepoints.

  14. AEs with relatedness associated with mefenamic acid

    Time frame: Up to Day 42

    Subjects will be continually monitored for adverse events

  15. AEs with relatedness associated with divalproex sodium ER

    Time frame: Up to Day 42

    Subjects will be continually monitored for adverse events

  16. AEs with relatedness associated with ecopipam

    Time frame: Up to Day 42

    Subjects will be continually monitored for adverse events

  17. Absolute values of white blood cell (WBC) count (K/Ul)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  18. Absolute values of neutrophils, lymphocytes, monocytes, eosinophils, and basophils (10E3/uL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  19. Absolute values of platelets (K/uL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  20. Absolute values of hematocrit (%)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  21. Absolute values of hemoglobin (g/dL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  22. Absolute values of Red blood cell (RBC) count (M/uL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  23. Absolute values of blood sodium, magnesium, urea, phosphorus, potassium, and chloride (mg/dL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of clinical chemistry parameters.

  24. Absolute values of creatinine, calcium, glucose, and direct and total bilirubin (mg/dL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of clinical chemistry parameters.

  25. Absolute values of albumin and total protein (g/dL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of clinical chemistry parameters.

  26. Absolute values of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), gamma glutamyl transferase (GGT), and creatinine phosphokinase (CPK)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of clinical chemistry parameters.

  27. Absolute values of urine specific gravity

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  28. Absolute values of urine pH

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  29. Absolute values of urine glucose

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  30. Absolute values of urine protein

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  31. Absolute values of urine blood

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  32. Absolute values of urine ketones

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  33. Absolute values of urine bilirubin, urobilinogen, and nitrite

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  34. Absolute values of urine leukocytes by dipstick

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  35. Change from Day -1 to Day of Discharge in white blood cell (WBC) count (K/Ul)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  36. Change from Day -1 to Day of Discharge in neutrophils, lymphocytes, monocytes, eosinophils, and basophils (10E3/uL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  37. Change from Day -1 to Day of Discharge in platelets (K/uL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  38. Change from Day -1 to Day of Discharge in hematocrit (%)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  39. Change from Day -1 to Day of Discharge in hemoglobin (g/dL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  40. Change from Day -1 to Day of Discharge in Red blood cell (RBC) count (M/uL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of hematology parameters.

  41. Change from Day -1 to Day of Discharge in blood sodium, magnesium, urea, phosphorus, potassium, and chloride (mg/dL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of clinical chemistry parameters.

  42. Change from Day -1 to Day of Discharge in creatinine, calcium, glucose, and direct and total bilirubin (mg/dL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of clinical chemistry parameters.

  43. Change from Day -1 to Day of Discharge in albumin and total protein (g/dL)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of clinical chemistry parameters.

  44. Change from Day -1 to Day of Discharge in alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), gamma glutamyl transferase (GGT), and creatinine phosphokinase (CPK) (U/L)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of clinical chemistry parameters.

  45. Change from Day -1 to Day of Discharge in urine specific gravity

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  46. Change from Day -1 to Day of Discharge in urine pH

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  47. Change from Day -1 to Day of Discharge in urine glucose

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  48. Change from Day -1 to Day of Discharge in urine protein

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  49. Change from Day -1 to Day of Discharge in urine blood

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  50. Change from Day -1 to Day of Discharge in urine ketones

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  51. Change from Day -1 to Day of Discharge in urine bilirubin, urobilinogen, and nitrite (Milligrams per deciliter)

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  52. Change from Day -1 to Day of Discharge in urine leukocytes by dipstick

    Time frame: Up to Day 17

    Urine samples will be collected for the assessment of urine parameters.

  53. Change from Day 6 to Day of Discharge in alanine aminotransferase (ALT) and aspartate aminotransferase (AST) (U/L)

    Time frame: Up to Day 17

    Blood samples will be collected for the assessment of clinical chemistry parameters.

  54. Absolute values of electrocardiogram (ECG) parameters: PR, QRS, QT, and QT interval corrected for heart rate using Fridericia's formula (QTcF) (Milliseconds)

    Time frame: Up to Day 10

    Twelve-lead ECGs will be obtained with the participant in a supine position after a rest of at least 5 minutes using an automated ECG machine. PR, QRS, QT, and QTcF intervals will be measured.

  55. Change from pre-dose for the respective day in ECG parameters: PR, QRS, QT, and QTcF (Milliseconds)

    Time frame: Up to Day 10

    Twelve-lead ECGs will be obtained with the participant in a supine position after a rest of at least 5 minutes using an automated ECG machine. PR, QRS, QT, and QTcF intervals will be measured.

  56. Absolute values of oral temperature (degrees Celsius)

    Time frame: Up to Day 17

    Temperature will be assessed as part of vital signs.

  57. Change from pre-dose for the respective day in oral temperature (degrees Celsius)

    Time frame: Up to Day 17

    Temperature will be assessed as part of vital signs.

  58. Absolute values of heart rate (beats/minute)

    Time frame: Up to Day 17

    Heart rate will be assessed as part of vital signs.

  59. Change from pre-dose for the respective day in heart rate (beats/minute)

    Time frame: Up to Day 17

    Heart rate will be assessed as part of vital signs.

  60. Absolute values of respiratory rate (breaths/minute)

    Time frame: Up to Day 17

    Respiratory rate will be assessed as part of vital signs.

  61. Change from pre-dose for the respective day in respiratory rate (breaths/minute)

    Time frame: Up to Day 17

    Respiratory rate will be assessed as part of vital signs.

  62. Absolute values of systolic blood pressure (SBP) and diastolic blood pressure (DBP) (mmHG)

    Time frame: Up to Day 17

    Blood pressure will be assessed as part of vital signs.

  63. Change from pre-dose for the respective day in SBP and DBP (mmHG)

    Time frame: Up to Day 17

    Blood pressure will be assessed as part of vital signs.

Sponsors and collaborators

Lead sponsor

Emalex Biosciences Inc.

Industry

Collaborators

  • Nuventra, Inc.
  • Syneos Health

Registry information

Official study title

A Phase 1, Open-Label, Fixed Sequence, Drug-Drug Interaction Study to Evaluate the Effect of Inhibition of Uridine 5'-Diphosphate-glucuronosyltransferases (UGTs) on the Pharmacokinetics of Ecopipam Tablets and Its Active Metabolite (EBS-101-40853) in Healthy Subjects

Important dates

Study start
2021
Primary completion
2021
Study completion
2021
First posted
May 26, 2021
Registry last updated
Jul 22, 2021

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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